143 articles for thisTarget
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Article Title
Organization
N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.
Boehringer Ingelheim Pharmaceuticals
Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.
Shandong University
Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.
Emory University
Exploration on natural product anibamine side chain modification toward development of novel CCR5 antagonists and potential anti-prostate cancer agents.
Virginia Commonwealth University
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Bristol-Myers Squibb
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.
Zhejiang University
Design, syntheses, and characterization of piperazine based chemokine receptor CCR5 antagonists as anti prostate cancer agents.
Virginia Commonwealth University
Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc.
The Scripps Research Institute
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.
Zhejiang University
Design, syntheses, and characterization of pharmacophore based chemokine receptor CCR5 antagonists as anti prostate cancer agents.
Virginia Commonwealth University
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication.
Sanofi
Targeting CCR2 Receptor To Treat Inflammation Diseases and Disorders.
Therachem Research Medilab (India)
Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.
Glaxosmithkline
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.
Glaxosmithkline
Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors.
University of Copenhagen
Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.
Bristol-Myers Squibb
Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.
TBA
Structure activity relationship studies of natural product chemokine receptor CCR5 antagonist anibamine toward the development of novel anti prostate cancer agents.
Virginia Commonwealth University
The potential role of anibamine, a natural product CCR5 antagonist, and its analogues as leads toward development of anti-ovarian cancer agents.
Virginia Commonwealth University
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity.
Astrazeneca
An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798).
Pfizer
Discovery of orally available spirodiketopiperazine-based CCR5 antagonists.
Minase Research Institute
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.
Chinese Academy of Sciences
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.
Roche Palo Alto
1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2.
Pfizer
1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1.
Pfizer
Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists.
K£Mia
Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.
Novartis Institutes For Biomedical Research
Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.
Ono Pharmaceutical
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
Ono Pharmaceutical
Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors.
Lindsley F. Kimball Research Institute
Inhibition of protein-protein association by small molecules: approaches and progress.
Pfizer
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.
Schering-Plough Research Institute
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements.
Merck Research Laboratories
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.
Astrazeneca
Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2).
Bristol-Myers Squibb
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Genzyme
Design and synthesis of a library of chemokine antagonists.
Novartis Institutes of Biomedical Research
The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents.
Virginia Commonwealth University
Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.
Ono Pharmaceutical
Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Genzyme
Discovery, optimization, and pharmacological characterization of novel heteroaroylphenylureas antagonists of C-C chemokine ligand 2 function.
Telik
Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.
TBA
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Incyte
Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.
Ono Pharmaceutical
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): optimization of the amine portion.
Glaxosmithkline
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.
Roche Palo Alto
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.
Chinese Academy of Sciences
Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier.
Institute of Materia Medica
Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.
Roche Palo Alto
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Genzyme
Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach.
Institute of Materia Medica
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.
Roche Palo Alto
Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles.
Minase Research Institute
Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.
Roche Palo Alto
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
Merck Research Laboratories
[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.
Glaxosmithkline
Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist.
Roche Palo Alto
Three-dimensional QSAR analyses of 1,3,4-trisubstituted pyrrolidine-based CCR5 receptor inhibitors.
Beijing University of Technology
Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum.
Schering-Plough Research Institute
Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea.
Merlion Pharmaceuticals
Isolation and structure of antagonists of chemokine receptor (CCR5).
Merck Research Laboratories
10-Methoxydihydrofuscin, fuscinarin, and fuscin, novel antagonists of the human CCR5 receptor from Oidiodendron griseum.
Merlion Pharmaceuticals
Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.
Merck Research Laboratories
CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives.
Berlex Biosciences
Identification of nonpeptide CCR5 receptor agonists by structure-based virtual screening.
Cnrs Umr 7175-Lc1
Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.
Merck Research Laboratories
CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives.
Berlex Biosciences
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Merck Research Laboratories
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Merck Research Laboratories
Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent Anti-HIV-1 activity.
Takeda Pharmaceutical
Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.
Astrazeneca
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
Takeda Pharmaceutical
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.
Shanghai Institute of Materia Medica
Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.
Astrazeneca
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Merck Research Laboratories
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
Pharmaceutical Research Institute
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.
Merck Research Laboratories
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.
Astrazeneca
Three new compounds from the plant Lippia alva as inhibitors of chemokine receptor 5 (CCR5).
Schering-Plough Research Institute
Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
Virginia Commonwealth University
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Merck Research Laboratories
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Merck Research Laboratories
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
Beijing Institute of Pharmacology and Toxicology
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagoni
Schering-Plough Research Institute
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.
Bristol Myers Squibb
Orally bioavailable competitive CCR5 antagonists.
Novartis Institutes For Biomedical Research
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Merck Research Laboratories
Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2.
Leiden Academic Centre For Drug Research
Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist.
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.
Schering-Plough Research Institute
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
Merck Research Laboratories
Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.
Virginia Commonwealth University
Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.
Schering-Plough Research Institute
Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Bristol Myers Squibb
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.
Merck Research Laboratories
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Merck Research Laboratories
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.
Merck Research Laboratories
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Merck Research Laboratories
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
Schering-Plough Research Institute
Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
Schering-Plough Research Institute
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted)piperidin-1-yl]butanes.
Merck Research Laboratories
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.
Schering-Plough Research Institute
Design, synthesis, and discovery of a novel CCR1 antagonist.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity.
Kyoto University
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Merck Research Laboratories
CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.
Smithkline Beecham Pharmaceuticals
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety.
Takeda Chemical Industries
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Bristol-Myers Squibb
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.
Leiden University
A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
Virginia Commonwealth University
Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.
Glaxosmithkline
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.
University of Chinese Academy of Sciences
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Design, synthesis and biological evaluation of (E)-3,4-dihydroxystyryl 4-acylaminophenethyl sulfone, sulfoxide derivatives as dual inhibitors of HIV-1 CCR5 and integrase.
Peking University
Recent updates for designing CCR5 antagonists as anti-retroviral agents.
Nirma University
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrido[4,3-c]azepin-5-one-based novel chemotype CCR2 antagonists via scaffold hopping strategy.
Shanghai Institute of Materia Medica
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase? (PI3K?) Inhibitors.
University Park Nottingham
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
Gsk Pharmaceuticals R & D
Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold.
Universit£T M£Nster
